Modulators of the glucocorticoid receptor and method

Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...

Reexamination Certificate

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Reexamination Certificate

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10865444

ABSTRACT:
Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structurewhere R1–R9, X, Y and Z are defined herein.

REFERENCES:
patent: 5688808 (1997-11-01), Jones et al.
patent: 5688810 (1997-11-01), Jones et al.
patent: 5693646 (1997-12-01), Jones et al.
patent: 5693647 (1997-12-01), Jones et al.
patent: 5696127 (1997-12-01), Jones et al.
patent: 5696130 (1997-12-01), Jones et al.
patent: 5696133 (1997-12-01), Jones et al.
patent: 6166013 (2000-12-01), Coghlan et al.
patent: 6358947 (2002-03-01), Zhi et al.
patent: 6380207 (2002-04-01), Coghlan et al.
patent: 6436985 (2002-08-01), Pinto
patent: 2001/0041802 (2001-11-01), Kym et al.
patent: 2001/0049377 (2001-12-01), Coghlan et al.
patent: WO 99/41256 (1999-08-01), None
patent: WO 01/16128 (2001-03-01), None
patent: WO 02/02565 (2002-01-01), None
Al-Dabbagh and Smith, “Species differences in oxidative drug metabolism: some basic considerations,” Archives of toxicology. Supplement. Archiv fur Toxikologie. supplement, vol. 7, pp. 219-231 (1984).
Hans Bundgaard, Design of Prodrugs, p. 1, © 1985 Elsevier Science Publishers.
Richard B. Silverman, The Organic Chemistry of Drug Design and Drug Action, pp. 352-400. © 1992 Academic Press, Inc.
Vippagunta et al, “Crystalline Solids” Advanced Drug Delivery Reviews, vol. 48, pp. 3-26 (2001).
Gavezzotti, “Are Crystal Structures Predictable?” Accounts of Chemical Research, vol. 27, pp. 309-314 (1994).
Reichardt et al, “Repression of inflammatory responses in the absence of DNA binding by the glucocorticoid receptor” The EMBO Journal, vol. 20(24), pp. 7168-7173 (2001).
Reichardt et al, “DNA Binding of the Glucocorticoid Receptor Is Not Essential for Survival” Cell, vol. 93, pp. 531-541 (1998).
Baldwin, Jr., A.S., “The transcription factor NF-κB and human disease”, The Journal of Clinical Investigation, vol. 107, No. 1, pp. 3-6 (2001).
Bamberger, C.M. et al., “Glucocorticoid Receptor β, a Potential Endogenous Inhibitor of Glucocorticoid Action in Humans”, The Journal of Clinical Investigation, vol. 95, pp. 2435-2441 (1995).
Brandon, D.D. et al., “Genetic variation of the glucocorticoid receptor from a steroid-resistant primate”, Journal of Molecular Endocrinology, vol. 7, pp. 89-96 (1991).
Caldenhoven, E. et al., “Negative Cross-Talk between RelA and the Glucocorticoid Receptor: A Possible Mechanism for the Antiinflammatory Action of Glucocorticoids”, Molecular Endocrinology, vol. 9, No. 4, pp. 401-412 (1995).
Chakravarti, D. et al., “Role CBP/P300 in nuclear receptor signaling”, Nature, vol. 383, pp. 99-103 (1996).
Danielsen, M. et al., “The mouse glucocorticoid receptor: mapping of functional domains by cloning, sequencing and expression of wild-type and mutant receptor proteins”, The EMBO Journal, vol. 5, No. 10, pp. 2513-2522 (1986).
Diamond, M.I. et al., “Transcription Factor Interactions: Selectors of Positive or Negative Regulation from a Single DNA Element”, Science, vol. 249, pp. 1266-1272 (1990).
Firestein, G.S. et al., “Signal Transduction and Transcription Factors in Rheumatic Disease”, Arthritis & Rheumatism, vol. 42, No. 4, pp. 609-621 (1999).
Hollenberg, S.M. et al., “Primary structure and expression of a functional human glucocorticoid receptor cDNA”, Nature, vol. 318, pp. 635-641 (1985).
Jonat, C. et al., “Antitumor Promotion and Antiinflammation: Down-Modulation of AP-1 (Fos/Jun) Activity by Glucocorticoid Hormone”, Cell, vol. 62, pp. 1189-1204 (1990).
Kamei, Y. et al., “A CBP Integrator Complex Mediates Transcriptional Activation and AP-1 Inhibition by Nuclear Receptors”, Cell, vol. 85, pp. 403-414 (1996).
Laudet, V. et al., The Nuclear Receptor FactsBook, Academic Press, publ., p. 345 (2002).
Miesfeld, R. et al., “Characterization of a steroid hormone receptor gene and mRNA in wild-type and mutant cells,” Nature, vol. 312, pp. 779-781 (1984).
Peltz, G., “Transcription factors in immune-mediated disease”, Current Opinion in Biotechnology, vol. 8, pp. 467-473 (1997).
Reichardt, H.M. et al., “DNA Binding of the Glucocorticoid Receptor Is Not Essential for Survival”, Cell, vol. 93, pp. 531-541 (1998).
Reichardt, H.M. et al., “Repression of inflammatory responses in the absence of DNA binding by the glucocorticoid receptor”, The EMBO Journal, vol. 24, No. 24, pp. 7168-7173 (2001).
Stöcklin, E. et al., “Functional interactions between Stat5 and the glucocorticoid receptor”, Nature, vol. 383, pp. 726-728 (1996).
Weinberger, C. et al., “Domain structure of human glucocorticoid receptor and its relationship to the v-erb-A oncogene product”, Nature, vol. 318, pp. 670-672 (1985).
Weinberger, C. et al., “Identification of Human Glucocorticoid Receptor Complementary DNA Clones by Epitope Selction”, Science, vol. 228, pp. 740-742 (1985).
Yang, K. et al., “Characterization of an ovine glucocorticoid receptor cDNA and developmental changes in its mRNA levels in the fetal sheep hypothalamus, pituitary gland and adrenal”, Journal of Molecular Endocrinology, vol. 8, pp. 173-180 (1992).
Yang-Yen, H.-F. et al., “Transcriptional Interference between c-Jun and the Glucocorticoid Receptor: Mutual inhibition of DNA Binding Due to Direct Protein—Protein Interaction”, Cell, vol. 62, pp. 1205-1215 (1990).
Zhi, L. et al., “5-Aryl-1,2,3,4-tetrahydrochromeno[3,4-f]quinolin-3-ones as a Novel Class of Nonsteroidal Progesterone Receptor Agonists: Effect of A-Ring Modification”, J. Med. Chem., vol. 42, No. 8, pp. 1466-1472 (1999).

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